GSK591 (Synonyms: EPZ015866; GSK3203591)

Name: GSK591
Brand: MedChemExpress
SKU: HY-100235
Rating: 5.0 (12 reviews)

Cat. No.: HY-100235 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC₅₀ of 4 nM.

For research use only. We do not sell to patients.

GSK591 Chemical Structure

CAS No. : 1616391-87-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 145	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 145	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 51	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 542	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 760	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of GSK591:

GSK591 hydrochloride Get quote

11 Publications Citing Use of MCE GSK591

Proliferation Assay

: GSK591 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]; GSK591 (PRMT5i; 200-1000 nM) in combination with EPZ020411 (PRMT6i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC₅₀ of 4 nM^[1].

IC₅₀ & Target

PRMT5

Cellular Effect

Cell Line	Type	Value	Description	References
Z-138	IC₅₀	62 nM Compound: EPZ015866; GSK3203591	Antiproliferative activity against human Z138 cells incubated for 5 days by cell titer-glo assay Antiproliferative activity against human Z138 cells incubated for 5 days by cell titer-glo assay	[PMID: 26985292]

In Vitro

GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	MCF7, T47D, and MCF10A cells
Concentration:	5 μM
Incubation Time:
Result:	Suppressed BCSCs proliferation and self-renewal.

Molecular Weight

380.48

Formula

C₂₂H₂₈N₄O₂

CAS No.

1616391-87-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(NC2CCC2)=NC=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (131.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6283 mL	13.1413 mL	26.2826 mL
5 mM	0.5257 mL	2.6283 mL	5.2565 mL
10 mM	0.2628 mL	1.3141 mL	2.6283 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (245 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. [1] Kenneth W. Duncan et al. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med. Chem. Lett., 2016, 7 (2), pp 162-166. [Content Brief]

[2]. Chiang K, et al. PRMT5 Is a Critical Regulator of Breast Cancer Stem Cell Function via Histone Methylation and FOXP1 Expression. Cell Rep. 2017 Dec 19;21(12):3498-3513. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6283 mL	13.1413 mL	26.2826 mL	65.7065 mL
	5 mM	0.5257 mL	2.6283 mL	5.2565 mL	13.1413 mL
	10 mM	0.2628 mL	1.3141 mL	2.6283 mL	6.5706 mL
	15 mM	0.1752 mL	0.8761 mL	1.7522 mL	4.3804 mL
	20 mM	0.1314 mL	0.6571 mL	1.3141 mL	3.2853 mL
	25 mM	0.1051 mL	0.5257 mL	1.0513 mL	2.6283 mL
	30 mM	0.0876 mL	0.4380 mL	0.8761 mL	2.1902 mL
	40 mM	0.0657 mL	0.3285 mL	0.6571 mL	1.6427 mL
	50 mM	0.0526 mL	0.2628 mL	0.5257 mL	1.3141 mL
	60 mM	0.0438 mL	0.2190 mL	0.4380 mL	1.0951 mL
	80 mM	0.0329 mL	0.1643 mL	0.3285 mL	0.8213 mL
	100 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6571 mL

GSK591 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK5911616391-87-7EPZ015866 GSK3203591GSK 591GSK-591EPZ 015866EPZ-015866GSK3203591GSK 3203591GSK-3203591Histone MethyltransferaseInhibitorinhibitorinhibit

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GSK591 (Synonyms: EPZ015866; GSK3203591)

Customer Review

Other Forms of GSK591:

GSK591 Related Antibodies

11 Publications Citing Use of MCE GSK591

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GSK591 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK591 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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